HIV Antivirals

Name Analogue|Derivative Function Notes

NRTI
Zidovudine (AZT|Retrovir) Thymidine Chain terminator
by cell enz to tri

TriAZT accum in uninfected cells
Granulocytopenia|anemia
Lamivudine (3TC|Epivir) Cytidine derivative Chain terminator
Competes with natural dCTP
Tx Chronic Hep B
Anemia
Didanosine (DDI|Videx) Dideoxy-inosine derivative Chain terminator
RT|compete with dATP
Inosine is a derivative of adenosine
Tx AZTHIV
D|N|V|Abd Pn|F|HA|rash
Periph neuropathy|pancreatitis
Emtricitabine (FTC) Cytidine RT|incorporate| Toxicity rare|D|N|HA|rash
Heptotoxicity|lactic acidosis
NtRTI
Tenofovir (TDF) Acyclic nucleoside phosphate of
adenosine
Targets viral RT|HBV RT Used in place of NRTI in
combination therapy
NNRTI
Nevirapine (Viramune) Allosterically bind NNRTI pocket nucleic acid synthesis cytochrome p450 isozymes
Hepatotoxicicty|fatal rash
Efavireneze (EFV|Efavir) Allosterically bind NNRTI pocket nucleic acid synthesis Never used alone
Use with Tenofovir/emtricitabine
Adults|Adolescents
Delavirdine (DLV|Respcriptor) - - efficacy|inconvenient schedule
p450 isozyme CYP3A4
RARELY used
Protease inhibitors
Ritonavir (Norvir) Induce & p450 (BD protease er)
blood triglyceride|D
Lopinavir (ABT-378) Fixed-dose combination with
Ritonavir (Kaletra)
Metabolized by liver|t1/2=5-6hrs
Fecal excretion|Highly prot bnd
Cross
induce resistance by them
Atazanavir (Reyataz)
Indinavir (Crixivan)
Saquinavir (Invirase)
Fusion Inhibitors
Enfuvirtide (Fuzeon)